1154426-01-3Relevant articles and documents
Ruthenium(II)-Catalyzed C-H (Hetero)Arylation of Alkenylic 1,n-Diazines (n = 2, 3, and 4): Scope, Mechanism, and Application in Tandem Hydrogenations
Gramage-Doria, Rafael,Achelle, Sylvain,Bruneau, Christian,Robin-Le Guen, Fran?oise,Dorcet, Vincent,Roisnel, Thierry
, p. 1462 - 1477 (2018/02/09)
A general ruthenium(II)-catalyzed methodology enabling the (hetero)arylation of alkenylic C-H bonds utilizing a series of synthetically appealing diazines as directing groups is presented. Despite the presence of additional nitrogen lone pairs remote from
Bis(arylvinyl)pyrazines, -pyrimidines, and -pyridazines As imaging agents for tau fibrils and β-Amyloid plaques in alzheimers disease models
Bolaender, Alexander,Kieser, Daniel,Voss, Constantin,Bauer, Silvia,Berger, Robert,Schmidt, Boris,Schoen, Christian,Burgold, Steffen,Bittner, Tobias,Herms, Jochen,Hoelzer, Jana,Hilger, Ingrid,Heyny-Von Haussen, Roland,Mall, Gerhard,Goetschy, Valerie,Czech, Christian,Knust, Henner
, p. 9170 - 9180,11 (2020/10/15)
The in vivo diagnosis of Alzheimers disease (AD) is of high socioeconomic interest and remains a demanding field of research. The biopathological hallmarks of the disease are extracellular plaques consisting of aggregated β-amyloid peptides (Aβ) and tau protein derived intracellular tangles. Here we report the synthesis and evaluation of fluorescent pyrazine, pyrimidine,and pyridazine derivatives in vitro and in vivo aiming at a tau-based diagnosis of AD. The probes were pre-evaluated on human brain tissue by fluorescence microscopy and were found to label all known disease-related alterations at high contrast and specificity. To quantify the binding affinity, a new thiazine red displacement assay was developed and selected candidates were toxicologically profiled. The application in transgenic mouse models demonstrated bioavailability and brain permeability for one compound. In the course of histological testing, we discovered an AD-related deposition of tau aggregates in the Bowmans glands of the olfactory epithelium, which holds potential for an endoscopic diagnosis of AD in the olfactory system.